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Inhibitor of fatty acid synthase and application thereof

A technology of fatty acid synthase and inhibitors, which is applied in the field of fatty acid synthase inhibitors, can solve the problems of limited application value and insufficient inhibitory activity, and achieve the effect of great application value

Inactive Publication Date: 2013-03-27
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The common disadvantage of these inhibitors is that the inhibitory activity is not high enough, and the application value is limited. Therefore, it is of great practical value to find fatty acid synthase inhibitors with high inhibitory activity in natural products.

Method used

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  • Inhibitor of fatty acid synthase and application thereof
  • Inhibitor of fatty acid synthase and application thereof
  • Inhibitor of fatty acid synthase and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1, the preparation of fatty acid synthase inhibitor

[0048] Wash the tea bar maple leaves collected in September in Jingbo Lake, Heilongjiang Province, dry them naturally or dry them at low temperature (<50°C) and pulverize them, and prepare fatty acid synthase inhibitors by the following method:

[0049] Use ethanol-water mixed solvent (the volume percentage of ethanol is 75%) to mix with the above-mentioned pulverized tea bar maple leaves in a mass and fraction ratio of 8:1, reflux at 78° C. for 1.5 hours, and filter; repeat the above-mentioned reflux operation for two times under the same conditions. times, filtered, and the three filtrates were combined. Evaporate and concentrate under reduced pressure and low temperature (0.09MPa, 55°C) to remove ethanol to obtain an aqueous phase containing effective substances, dissolve it with an appropriate amount of methanol, and then extract with an equal volume of petroleum ether (boiling point 60-90°C) for 3-4 t...

Embodiment 2

[0124] Embodiment 2, the detection of FAS inhibitory activity of fatty acid synthase inhibitor of the present invention

[0125] NADPH, acetyl-CoA, malonyl-CoA, and DTT (dithiothreitol) used in the test were all purchased from Roche Diagnostics.

[0126] At 37°C, add FAS substrates to a 2ml quartz cuvette: 25μl of 0.2mM acetyl-CoA solution, 50μl of 0.4mM malonyl-CoA solution and 50μl of 1.3mM NADPH solution, then add 0.1M pH7. Mix 1.85ml of 0 phosphate buffer solution and 25μl of FAS solution to start the enzymatic reaction. The activity of FAS was expressed by detecting the change (ΔA / min) of the absorbance value A at a wavelength of 340nm per unit time with a spectrophotometer. In the presence of the fatty acid synthase inhibitor solution prepared in a certain concentration embodiment 1, the activity of the FAS holoenzyme reaction decreases, and the concentration of the required fatty acid synthase inhibitor when its activity drops by half is IC 50 , using this value to re...

Embodiment 3、 5

[0134] Example 3, Detection of FAS Inhibitory Activities of Pentagalloyl Gluconic Acid, Methyl Gallate and Drobetin-3-O-L-Rhamnoside

[0135] The specific determination method is the same as the detection of the inhibitory activity of fatty acid synthase inhibitors on FAS in Example 2.

[0136] Preparation of pentagalloyl gluconic acid solution: 16.8 mg of pentagalloyl gluconic acid isolated in Example 1 was dissolved in 1 ml of methanol to obtain a pentagalloyl gluconic acid solution with a concentration of 16.8 mg / ml.

[0137] Preparation of methyl gallate solution: 16 mg of the methyl gallate isolated in Example 1 was dissolved in 1 ml of methanol to obtain a methyl gallate solution with a concentration of 16 mg / ml.

[0138] Preparation of the dendrobetin-3-O-L-rhamnoside solution: 20 mg of the dendrobetin-3-O-L-rhamnoside isolated in Example 1 was dissolved in 1 ml of methanol to obtain dendrobite with a concentration of 20 mg / ml Prime-3-O-L-rhamnoside solution.

[0139]...

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Abstract

The invention discloses an inhibitor of fatty acid synthase and application thereof, comprising the following active ingredients: 5 galloyl group gluconic acid, methyl gallate and quercetin-3-O-L-rhamnoside. The mass of three active ingredients in per gram of the inhibitor of fatty acid synthase are sequentially as follows: 18-20mug, 2-3mug, 1-2mug. The inhibitor of fatty acid synthase not only can be applied to preparation of weight loss drugs, preparation of anti-cancer drugs, but also can be widely applied to additives for foods, health products, as well as daily chemicals.

Description

technical field [0001] The invention relates to a fatty acid synthase inhibitor and its application. Background technique [0002] Fatty acid synthase (EC2.3.1.85, fatty acid synthase, abbreviated as FAS) is an important enzyme for the synthesis of endogenous fatty acids. It is a macromolecular protein complex with 7 enzyme activities. Fatty acid synthase in animals is called type I FAS, and fatty acid synthase in prokaryotes and plants is called type II FAS. Basic research at home and abroad has shown that fatty acid synthase has become a potential target for weight loss and tumor suppression. [0003] So far, there are few fatty acid synthase inhibitors reported, only synthetic C75 (Kuhajda F.P., Pizer E.S., LiJ.N., et al.Proc Natl Acad Sci USA, 97, 3450-3454 (2000)), compared with The early discovered natural product cerulenin (cerulenin) (Vance D., Goldberg I., Mitsuhashi O. et al. Biochem Biophys Res Commun. 48, 649-656 (1972)) and the ester type catechin EGCG in gree...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C69/84C07D311/30A61K31/235A61K31/352A61P35/00A61P3/04
Inventor 李珺赵光孙彬屈爱桃宋丰宇李教社
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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